US8802734B2ActiveUtilityA1

Method of treating or preventing pain

80
Assignee: KAPLAN ELIAHUPriority: Sep 9, 2009Filed: Sep 9, 2010Granted: Aug 12, 2014
Est. expirySep 9, 2029(~3.2 yrs left)· nominal 20-yr term from priority
Inventors:Eliahu Kaplan
A61K 31/165C07C 233/22A61K 31/315A61K 9/0053A61P 29/00C07F 3/06
80
PatentIndex Score
2
Cited by
82
References
20
Claims

Abstract

Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula I: in which: the dotted line represents a single or a double bond; and R 5 and R 5 ′ are independently —H, —OH or —OR 6 , where R 6 is a linear or branched C 1 -C 4 alkyl; X is —CH 2 O—; Z is —CH 2 CH 2 O—, —CH(CH 3 )CH 2 O— or —CH 2 CH(CH 3 )O—; m is 1; and n is an integer of 1-5. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.

Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. A method for treating nociceptive pain selected from somatic, visceral, and myofascial or edema in a human or non-human animal patient in need thereof, which method comprises administering to said patient a therapeutically effective amount of at least one compound represented by formula I: 
       
         
           
           
               
               
           
         
         wherein: 
            represents a single or a double bond; 
         R 5  and R 5 ′ are independently —H, —OH or —OR 6 , wherein R 6  is a linear or branched C 1 -C 4  alkyl; 
         X is —CH 2 O—; 
         Z is —CH 2 CH 2 O—, —CH(CH 3 )CH 2 O— or —CH 2 CH(CH 3 )O—; 
         m is 1; and 
         n is an integer of 1, 2, 3, 4, or 5; 
         or a pharmaceutically acceptable salt, prodrug, metabolite, or hydrate thereof. 
       
     
     
       2. The method as claimed in  claim 1  for the treatment of acute or chronic nociceptive pain. 
     
     
       3. The method as claimed in  claim 1 , wherein the compound is represented by formula III: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, prodrug, metabolite, or hydrate thereof. 
       
     
     
       4. The method as claimed in  claim 1 , wherein R 5  is H or OH. 
     
     
       5. The method as claimed in  claim 1 , wherein R 5 ′ is H or OH. 
     
     
       6. The method as claimed in  claim 3 , wherein n is 1 or 2. 
     
     
       7. The method as claimed in  claim 1 , wherein the compound is represented by formula IV, V, VI or VII: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, prodrug, metabolite, or hydrate thereof, 
         wherein R is a polyalkylene glycol polymer having n units, wherein n is an integer of 1, 2, 3, 4, or 5. 
       
     
     
       8. The method as claimed in  claim 1 , wherein the compound is administered as a pharmaceutical composition comprising a therapeutically effective amount of one or more of the compounds represented by formula I together with one or more pharmaceutically acceptable excipients. 
     
     
       9. The method as claimed in  claim 1  for the treatment of somatic pain or visceral pain, wherein said somatic pain originates from tendons, bones, blood vessels or nerves. 
     
     
       10. The method as claimed in  claim 9  for the treatment of phantom limb pain. 
     
     
       11. The method as claimed in  claim 1  for the treatment of edema. 
     
     
       12. The method as claimed in  claim 1 , wherein the compound is selected from 
       
         
           
           
               
               
           
         
       
     
     
       13. The method as claimed in  claim 9  for the treatment of headache. 
     
     
       14. A method for treating somatic pain, visceral pain, myofascial pain, or edema in a human patient in need thereof, which method comprises administering to said patient a therapeutically effective amount of the compound: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
       15. The method as claimed in  claim 14  for the treatment of somatic pain, wherein said somatic pain originates from tendons, bones, blood vessels or nerves. 
     
     
       16. The method as claimed in  claim 15  for the treatment of headache. 
     
     
       17. The method as claimed in  claim 14  for the treatment of visceral pain. 
     
     
       18. The method as claimed in  claim 14  for the treatment of phantom limb pain. 
     
     
       19. The method as claimed in  claim 14  for the treatment of myofascial pain. 
     
     
       20. The method as claimed in  claim 10  for the treatment of edema.

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